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Asapiprant

Catalog No. T5386Cas No. 932372-01-5

Asapiprant (S-555739) is a potent and selective DP1 receptor antagonist (Ki: 0.44 nM). It exhibited high affinity and selectivity for the DP1 receptor.

Asapiprant

Asapiprant

Purity: 99.64%
Catalog No. T5386Cas No. 932372-01-5
Asapiprant (S-555739) is a potent and selective DP1 receptor antagonist (Ki: 0.44 nM). It exhibited high affinity and selectivity for the DP1 receptor.
Pack SizePriceAvailabilityQuantity
1 mg$34In Stock
5 mg$98In Stock
10 mg$158In Stock
25 mg$298In Stock
50 mg$472In Stock
100 mg$768In Stock
200 mg$987In Stock
1 mL x 10 mM (in DMSO)$107In Stock
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Purity:99.64%
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Product Introduction

Bioactivity
Description
Asapiprant (S-555739) is a potent and selective DP1 receptor antagonist (Ki: 0.44 nM). It exhibited high affinity and selectivity for the DP1 receptor.
Targets&IC50
DP1 receptor:0.44 nM (Ki)
In vitro
Asapiprant strongly inhibited the cAMP elevation elicited by PGD2 in human platelets with a half-maximal inhibitory concentration (IC50) value of 16 nM. Strong inhibition by asapiprant was observed in the cAMP elevation induced by PGD2 in guinea pigs, rats, and sheep with IC50 values (nM) of 61, 74, and 15, respectively.
In vivo
Intranasal challenge with 0.5% PGD2 led to a rapid increase in nasal resistance (sRaw) from 5 min to 60 min in sensitized guinea pigs. Oral administration of asapiprant at 1 and 3 mg/kg significantly suppressed the increase in nasal resistance by 82% and 92%, respectively. By contrast, S-5751 showed partial suppression on PGD2-induced nasal resistance in guinea pigs at 30 mg/kg by 76% that was inferior to the suppression by asapiprant at 3 mg/kg.
Cell Research
The functional antagonist activity of asapiprant on the DP1 receptor was evaluated by examining PGD2-induced elevation of cyclic adenosine monophosphate (cAMP) in platelet-rich plasma derived from venous blood (humans, guinea pigs, and sheep), and in rat DP1-transfected cells stimulated with PGD2, as described elsewhere. The functional antagonist activity of asapiprant on the DP2 receptor was evaluated by examining PGD2-induced shape change of peripheral eosinophils derived from humans and guinea pigs, as reported previously.
Animal Research
After the oral administration of asapiprant or S-5751 to rats, guinea pigs, dogs, and sheep at 10 mg/kg in suspension with 0.5% methylcellulose solution, the plasma concentrations of the drugs were measured by liquid chromatography/tandem mass spectrometry or high-performance liquid chromatography.
Chemical Properties
Molecular Weight501.55
FormulaC24H27N3O7S
Cas No.932372-01-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 10 mg/mL (19.94 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9938 mL9.9691 mL19.9382 mL99.6910 mL
5 mM0.3988 mL1.9938 mL3.9876 mL19.9382 mL
10 mM0.1994 mL0.9969 mL1.9938 mL9.9691 mL

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